产品
编 号：F741529
分子式：C33H31ClN2O4
分子量：555.06
分子式：C33H31ClN2O4
分子量：555.06
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2377916-66-8
产品详情
生物活性：
PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
体内研究：
PD-1/PD-L1-IN-NP19 (compound NP19) (25-100 mg/kg; intragastric gavage once daily for 15 d) inhibits the growth of melanoma tumors dramatically in mice.PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 d) demonstrates significant antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well tolerated in an H22 hepatoma mouse model.PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t1/2=1.5±0.5 h), clearance rate (CL=0.9±0.2 L/h/kg) and apparent distribution volume (Vss=2.1±0.5 L/kg) in rats.PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (Tmax=0.6±0.2 h), long half-life (t1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats.Animal Model:BALB/c mice (6-8 weeks) with B16-F10 melanoma tumors
Dosage:25, 50, 100 mg/kg
Administration:Intragastric gavage once daily for 15 days
Result:Inhibited the growth of melanoma tumors up to 51.1, 75 and 80.9% at dose of 25, 50, 100 mg/kg, respectively.Exhibited normal physical activity and increased body weights slightly.
Animal Model:Male Sprague-Dawley rats
Dosage:1 mg/kg for i.v. and 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:I.v. and p.o.
Result:I.v.: t1/2=1.5 h; Cmax=1751 μg/L; CL=0.9 L/h/kg.P.o.: t1/2=10.9 h; Cmax=69.5 μg/L; CL=23.1 L/h/kg.
体外研究：
PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates the production of IFN-γ in a dose dependent manner from T cells co-cultured with tumor cells.PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC50 in the micromolar range (>1μM), as compared to the inhibition of human PD1/PD-L1 interaction (IC50=12.5 nM).PD-1/PD-L1-IN-NP19 (10 μM; 48 h) displays no apparent cytotoxic effects on A549, MCF-7, and B16-F10 cells at a concentration of 10 μM.
PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
体内研究：
PD-1/PD-L1-IN-NP19 (compound NP19) (25-100 mg/kg; intragastric gavage once daily for 15 d) inhibits the growth of melanoma tumors dramatically in mice.PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 d) demonstrates significant antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well tolerated in an H22 hepatoma mouse model.PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t1/2=1.5±0.5 h), clearance rate (CL=0.9±0.2 L/h/kg) and apparent distribution volume (Vss=2.1±0.5 L/kg) in rats.PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (Tmax=0.6±0.2 h), long half-life (t1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats.Animal Model:BALB/c mice (6-8 weeks) with B16-F10 melanoma tumors
Dosage:25, 50, 100 mg/kg
Administration:Intragastric gavage once daily for 15 days
Result:Inhibited the growth of melanoma tumors up to 51.1, 75 and 80.9% at dose of 25, 50, 100 mg/kg, respectively.Exhibited normal physical activity and increased body weights slightly.
Animal Model:Male Sprague-Dawley rats
Dosage:1 mg/kg for i.v. and 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:I.v. and p.o.
Result:I.v.: t1/2=1.5 h; Cmax=1751 μg/L; CL=0.9 L/h/kg.P.o.: t1/2=10.9 h; Cmax=69.5 μg/L; CL=23.1 L/h/kg.
体外研究：
PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates the production of IFN-γ in a dose dependent manner from T cells co-cultured with tumor cells.PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC50 in the micromolar range (>1μM), as compared to the inhibition of human PD1/PD-L1 interaction (IC50=12.5 nM).PD-1/PD-L1-IN-NP19 (10 μM; 48 h) displays no apparent cytotoxic effects on A549, MCF-7, and B16-F10 cells at a concentration of 10 μM.
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